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Active ingredient: Ethinyl Estradiol - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Estrogens

Dosage Forms

  • Disc (sustained-release)
  • Gel
  • Implant
  • Liquid
  • Patch
  • Ring (slow-release)
  • Solution
  • Tablet

Brands / Synonyms

17 alpha-Ethinylestradiol; 17 alpha-Ethynylestradiol; 17 alpha-Ethynyloestradiol; Aethinyloestradiolum; Aethinyoestradiol [German]; Alesse; Alora; Amenoron; Amenorone; Anovlar; Binovum; Brevicon; Brevinor; Climara; Conceplan; Cyclosa; Demulen; Desogen; Dicromil; Diognat-E; Diogyn E; Diogyn-E; Diprol; Dyloform; EE; EE2; EO; Ertonyl; Esclim; Esteed; Estigyn; Estinyl; Eston-E; Estopherol; Estoral; Estoral {[Orion]}; Estorals; Estrace; Estraderm; Estradiol; Estring; Estrogel; Estrogen; Ethidol; Ethinoral; Ethinyl-Oestranol; ETHINYLESTRADIOL; Ethinylestradiolum [Inn-Latin]; Ethinylestriol; Ethinyloestradiol; Ethy 11; Ethynylestradiol; Ethynyloestradiol; Eticyclin; Eticyclol; Eticylol; Etinestrol; Etinestryl; Etinilestradiol [Inn-Spanish]; Etinilestradiolo [Dcit]; Etinoestryl; Etistradiol; Etivex; Femhrt; Feminone; Fempatch; Follicoral; Genora; Ginestrene; Gynodiol; Gynolett; Halodrin; Inestra; Innofem; Jenest; Kolpolyn; Leena; Levlen; Levlite; Linoral; LO Ovral; Lo/Ovral; Loestrin; Logynon; Lybrel; Lynoral; Marvelon; Menolyn; Menostar; Mercilon; Microfollin; Microgynon; Mircette; Modicon; Necon; NEE; Nelova; Neo-Estrone; Neocon; Nogest-S; Norcept; Nordette; Norethin 1/35 E; Norimin; Norinyl; Norlestrin; Novestrol; Nuvaring; Oradiol; Orestralyn; Orestrayln; Ortho; Ortho TRI-Cyclen; Ortho TRI-Cyclen LO; Ortho-Cept; Ortho-Cyclen; Ortho-Novum; Ovcon; Ovex; Oviol; Ovral; Ovran; Ovranette; Ovysmen; Palonyl; Perovex; Primogyn; Primogyn C; Primogyn M; Progynon C; Progynon M; Prosexol; Seasonale; Spanestrin; Stediril; Synphase; Tetragynon; Thiuram E; Thiuranide; Tri-Levlen; Tri-Norinyl; Trinordiol; Trinovum; Triphasil; Vagifem; Varnoline; Vivelle; Yasmin; Ylestrol


For treatment of moderate to severe vasomotor symptoms associated with the menopause, female hypogonadism, prostatic carcinoma-palliative therapy of advanced disease, breast cancer, as an oral contraceptive, and as emergency contraceptive.


Ethinyl estradiol is a synthetic derivative of the natural estrogen estradiol. It is one of two estrogens currently used in oral contraceptive pills. The other, mestranol, is converted to ethinyl estradiol before it is biologically active. Ethinyl estradiol and norethindrone are used together as an oral contraceptive agent.

Mechanism of Action

Estrogens diffuse into their target cells and interact with a protein receptor. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system, decreasing the secretion of gonadotropin-releasing hormone (GnRH).


Rapid and complete absorption follows oral intake of ethinyl estradiol (bioavailability 43%).


Oral, mouse LD50: 1737 mg/kg. Symptoms of overdose include nausea and vomiting, and withdrawal bleeding may occur in females.

Biotrnasformation / Drug Metabolism

Hepatic. Quantitatively, the major metabolic pathway for ethinyl estradiol, both in rats and in humans, is aromatic hydroxylation, as it is for the natural estrogens.


Estrogens should not be used in women (or men) with any of the following conditions:

1. Known or suspected cancer of the breast except in appropriately selected patients being treated for metastatic disease.

2. Known or suspected estrogen-dependent neoplasia.

3. Known or suspected pregnancy.

4. Undiagnosed abnormal genital bleeding.

5. Active thrombophlebitis or thromboembolic disorders.

6. A past history of thrombophlebitis, thrombosis, or thromboembolic disorders associated with previous estrogen use (except when used in treatment of breast or prostatic malignancy).

Drug Interactions

Certain endocrine and liver function tests may be affected by estrogen-containing oral contraceptives. The following similar changes may be expected with larger doses of estrogen:

Increased sulfobromophthalein retention; increased prothrombin and factors VII, VIII, IX, and X; decreased antithrombin 3; increased norepinephrine-induced platel et aggregation; increased thyroid binding globulin (TBG) leading to increased circulating total thyroid hormone, as measured by PBI, T4 by column, or T4 by radioimmunoassay. Free T3 resin uptake is decreased, reflecting the elevated TBG; free T4 concentration is unaltered: impaired glucose tolerance; decreased pregnanediol excretion; reduced response to metyrapone test; reduced serum folate concentration; increased serum triglyceride and phospholipid concentration.

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